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Chemical Structure : MI-3454
Catalog No.: PC-72046Not For Human Use, Lab Use Only.
MI-3454 (MI 3454) is a highly potent, orally bioavailable inhibitor of the menin-MLL1 interaction with IC50 of 0.51 nM, 60-fold improvement over MI-503.
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MI-3454 (MI 3454) is a highly potent, orally bioavailable inhibitor of the menin-MLL1 interaction with IC50 of 0.51 nM, 60-fold improvement over MI-503.
MI-3454 inhibits growth of human MLL leukemic cell lines (MLL-tr): MV-4-11, MOLM-13, KOPN-8, SEM, RS4-11 with GI50 values of 7-27 nM in MTT cell viability assays, does not significantly (>100-fold) affect the growth of leukemic cells without MLL1 translocations.
MI-3454 (50 nM or lower) led to downregulated expression of HOXA9 and MEIS1 in MV-4-11 and MOLM13 cells, also reduced other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.
MI-3454 demonstrated strong reduction of cell proliferation and downregulation of HOXA9 and MEIS1 expression in mouse bone marrow cells transformed with the MLL-AF9 oncogene but not in bone marrow cells transformed with HOXA9 and MEIS1 oncogenes.
MI-3454 induces leukemia regression in xenograft model of MLL leukemia through on-target activity.
MI-3454 (3–12 nM) substantially reduced clonogenic potential in MLL leukemia patient samples with MLL1 translocations or NPM1 mutations, MI-3454 induced complete remission or blocks leukemia progression in PDX models of MLL leukemia.
| M.Wt | 636.742 | |
| Formula | C32H35F3N8OS | |
| Appearance | Solid | |
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1. Klossowski S, et al. J Clin Invest. 2020 Feb 3;130(2):981-997.
2. Miao H, et al. Blood. 2020 Dec 17;136(25):2958-2963.
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